Resp Drugs Flashcards

1
Q

What is the mechanism of a beta-2-adrenoceptor agonist?

A

beta 2 receptors are coupled with Gs proteins

Agonist binding stimulates adenylyl cyclase which converts ATP into cAMP

Phosphodiesterase breaks down cAMP

Decrease intracellular Ca levels and increase formation of protein kinase A

Protein kinase A phosphorylates myosin light chain kinase which brings about relaxation of bronchi smooth muscle

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2
Q

What is an example of a SABA?

A

Salbutamol

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3
Q

Example of a LABA?

A

Salmeterol

Formoterol

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4
Q

What are side effects of beta-2-agonists?

A

Fine tremor
Hypotension
Tachycardia

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5
Q

Where are CysLTs derived from?

A

Mast cells

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6
Q

Explain the mechanism behind leukotriene release form mast cells.

A

Mast cells produce arachidonic acid by stimulation of phospholipase A2
Stimulation of 5-lopooxygenase by FLAP enzyme
Release of leukotirienes which bind to CysLT1

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7
Q

CysLT1 Antagonists prevent?

A

Muscle contraction, mucous secretion and oedema

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8
Q

What are examples of CysLT1 receptor antagonists?

A

Montelukast

Zafirlukast

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9
Q

What are side effects of CysLT1 Receptor Antagonists?

A

Abdominal Pain

Headaches

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10
Q

What are examples of xanthines?

A

Theophylline

Aminophylline

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11
Q

What is the mechanism of xanthines?

A

Inhibit phosphodiesterase which increases cAMP levels (breakdown of cAMP in inhibited)

Decreases protein kinase A

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12
Q

What are side effects of xanthines?

A

Nausea
Vomiting
Abdominal discomfort
Headache

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13
Q

What is the mechanism of a corticosteroid?

A

Signalling via nuclear receptors GR-alpha where glucocorticoid binds and enters the nucleus
Binds to promotor region and either produces transactivation or trans repression of genes the control inflammation

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14
Q

Which genes are induced by corticosteroids?

A

Annexin 1 - inhibits synthesis of phospholipase A1

Decrease formation of arachidonic acid and decreases production of leukotrienes, chemotaxis and spasmogens

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15
Q

Which genes are repressed by corticosteroids?

A

Cytokines
Decrease formation of IL 4, 5, 7, and 13
Eosinophils and plasma cells (IgE) are not recruited

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16
Q

What are side effects of corticosteroids?

A
Oropharyngeal candidiasis (thrush)
Dysphonia (hoarse and weak voice)
Growth restrictions
Glaucoma
Diabetes
Cushing's syndrome
17
Q

What is an example of a cromone?

A

Cromoglicate

18
Q

What is an example of an oral corticosteroid?

A

Prednisolone

19
Q

What is an example of an inhaled corticosteroid?

A

Beclometasone

20
Q

What is the mechanism of cromoglicate?

A

Decreases sensitivity of exposed C-fibres in endothelium

21
Q

What are side effects of corticosteroidsß

A

Local irritation

22
Q

What is Omalizumab?

A

Monoclonal antibody against IgE

23
Q

What are side effects of Omalizumab?

A

Abdominal pain

Pyrexia

24
Q

Ipratropium is an example of a?

A

Short acting muscarinic ACh Antagonist of M3 receptors

25
Q

What mechanism does a muscarinic ACh antagonist of M3 receptors prevent?

A
Activated M3 acts on Gq coupled protien
Increase formation of phospholipase C
Pip2 degrades phospholipase C into IP3
Calcium is released
Smooth muscle of bronchi contracts
26
Q

What are side effects of muscarinic antagonists?

A
Dry mouth 
Dizziness
Oropharyngeal
Candidiasis
Taste disturbance
27
Q

What is an example of an anti-histamine?

A

Loratadine

28
Q

What is the mechanism of an anti-histamine?

A

Reduce effects of mast cell activation

29
Q

What are the side effects of anti-histamines?

A

Drowsiness
Palpitations
Hypotension

30
Q

What s an example of a vasoconstrictor?

A

Oxymetazoline

31
Q

What is the mechanism of Oxymetazoline?

A

mimics effects of noradrenaline (alpha-1-agonist)

32
Q

What are the side effects of oxymetazoline?

A

Rhinitis medicamentosa (nasal congestion caused by desensitisation of receptors once drugs are discontinued)